反应详情

温度

25 °C

{5-[(5-{[(4-chlorophenyl)acetyl]amino}pyridin-3-yl)carbonyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl}acetic acid potassium salt (Example 307, 50 mg, 0.102 mmol) was added to a stirred solution of dimethyl amine HCl (12.5 mg, 0.153 mmol) and HATU (58.2 mg, 0.153 mmol) in pyridine (2 mL) and the resultant solution was stirred at 50° C. (reactivial) for 14 hours. The reaction was cooled to 25° C., diluted with DCM (5 mL) then quenched with saturated NaHCO3 (aq) (5 mL) and extracted with further DCM (3×5 mL). The organics were combined, washed with saturated brine (5 mL), dried over anhydrous magnesium sulfate and concentrated in vacuo. Purification by preparative HPLC gave the title compound in 55% yield, 26.6 mg.

1. customthen quenched with saturated NaHCO3 (aq) (5 mL)
2. extractionextracted with further DCM (3×5 mL)
3. washwashed with saturated brine (5 mL)
4. dry with materialdried over anhydrous magnesium sulfate
5. concentrationconcentrated in vacuo
6. customPurification by preparative HPLC